A CSF1R inhibitor
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Alternative(s)
36277PLX5622 (hemifumarate)
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PLX5622

Item No. 28927

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-fluoro-N-[6-fluoro-5-[(5-methyl-1H-pyrrolo[2,3-b]pyridin-3-yl)methyl]-2-pyridinyl]-2-methoxy-3-pyridinemethanamine
CAS Number
1303420-67-8
Molecular Formula
C21H19F2N5O
Formula Weight
395.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 5 mg/mLDMSO: 5 mg/mLDMSO:PBS (pH 7.2) (1:3): 0.2 mg/mL
λmax
227, 291 nm
SMILES
CC1=CN=C(NC=C2CC3=C(F)N=C(NCC4=C(OC)N=CC(F)=C4)C=C3)C2=C1
InChi Code
InChI=1S/C21H19F2N5O/c1-12-5-17-14(9-26-20(17)25-8-12)6-13-3-4-18(28-19(13)23)24-10-15-7-16(22)11-27-21(15)29-2/h3-5,7-9,11H,6,10H2,1-2H3,(H,24,28)(H,25,26)
InChi Key
NSMOZFXKTHCPTQ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    5 mg

    $95

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    10 mg

    $152

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    25 mg

    $238

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    50 mg

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    Product Description

    PLX5622 is a brain-penetrant inhibitor of the colony stimulating factor 1 receptor (CSF1R; IC50 = 0.016 µM).1 It is selective for CSF1R over FMS-related tyrosine kinase 3 (FLT3), Kit, Aurora C, and kinase insert domain receptor (VEGFR2; IC50s = 0.39, 0.86, 1, and 1.1 µM, respectively) and is greater than 100-fold selective for CSF1R over a panel of 230 kinases.1,2 PLX5622 (65 mg/kg) reduces the number of Iba-1+ cells, a marker of reduced microglia activation, in the dorsal horn of the spinal cord in a mouse model of neuropathic pain induced by partial ligation of the sciatic nerve.2 It also decreases macrophage levels of TNF-α and IL-1β and infiltration into the sciatic nerve, as well as alleviates mechanical and cold allodynia in the same model. Dietary administration of PLX5622 (1,200 ppm in chow) decreases the number of hippocampal microglia by 90%, as well as reduces the number and volume of retrosplenial and somatosensory cortical amyloid-β (Aβ) plaques in the 5XFAD transgenic mouse model of Alzheimer's disease.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Spangenberg, E., Severson, P.L., Hohsfield, L.A., et al. Sustained microglial depletion with CSF1R inhibitor impairs parenchymal plaque development in an Alzheimer’s disease model. Nat. Commun. 10(1), 3758 (2019).

    2. Lee, S., Shi, X.Q., Fan, A., et al. Targeting macrophage and microglia activation with colony stimulating factor 1 receptor inhibitor is an effective strategy to treat injury-triggered neuropathic pain. Mol. Pain 14, (2018).

    Product Citations

    Callahan, A., Zhang, X., Wang, A., et al. CSF1R-CAR T cells induce CSF1R signaling and can promote target cell proliferation. Sci. Signal. 18(912), eadv4112 (2025).

    Wu, J., Zhang, J., and Lin, B. Dual-targeting CSF1R signaling attenuates neurotoxic myeloid activation and preserves photoreceptors in retinitis pigmentosa. J. Neuroinflammation 22, 193 (2025).

    Xu, H., Lotfy, P., Gelb, S., et al. The choroid plexus synergizes with immune cells during neuroinflammation. Cell 187(18), 4946-4963 (2024).